Collagen proline hydroxylase inhibitor - CAS 223666-07-7
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Not Intended for Therapeutic Use. For research use only.
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Collagen proline hydroxylase inhibitor is a collagen proline hydroxylase inhibitor; useful for antifibroproliferative agents.
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1,10-Phenanthroline-3-carboxamide, N-ethyl-7,10-dihydro-8-nitro-7-oxo-N-propyl-
1.Mechanical stretch promotes matrix metalloproteinase-2 and prolyl-4-hydroxylase α1 production in human aortic smooth muscle cells via Akt-p38 MAPK-JNK signaling.
Liu X1, Huang X1, Chen L2, Zhang Y1, Li M1, Wang L1, Ge C1, Wang H1, Zhang M3. Int J Biochem Cell Biol. 2015 May;62:15-23. doi: 10.1016/j.biocel.2015.02.009. Epub 2015 Feb 21.
Hypertension can increase mechanical stretch on the vessel wall, an important stimulus that induces collagen remodeling. Prolyl-4-hydroxylaseα1 (P4Hα1) and matrix metalloproteinases (MMPs) are essential for collagen synthesis and degradation. However, the effect of mechanical strain and collagen synthesis remains largely unknown. This study aimed to identify the effect of stretch on MMPs and P4Hα1 and the involved signaling pathways. Human aortic smooth muscle cells (HASMCs) were stimulated with mechanical stretch (0, 10% and 18% strain), and production of P4Hα1 as well as production and gelatinolytic activity of MMP-2 was force-dependently increased. Mechanical stretch at 18% also increased the expression of type I and III collagen and the phosphorylation of Akt, p38 mitogen-activated protein kinase (MAPK) and c-Jun N-terminal kinase (JNK). MMP-2 production and activity enhanced by 18% stretch were inhibited by the PI3K/Akt inhibitor LY294002.
2.Selective Inhibition of Collagen Prolyl 4-Hydroxylase in Human Cells.
Vasta JD1, Andersen KA2, Deck KM3, Nizzi CP3, Eisenstein RS3, Raines RT1,4. ACS Chem Biol. 2016 Jan 15;11(1):193-9. doi: 10.1021/acschembio.5b00749. Epub 2015 Nov 19.
Collagen is the most abundant protein in animals. Its overproduction is associated with fibrosis and cancer metastasis. The stability of collagen relies on post-translational modifications, the most prevalent being the hydroxylation of collagen strands by collagen prolyl 4-hydroxylases (CP4Hs). Catalysis by CP4Hs enlists an iron cofactor to convert proline residues to 4-hydroxyproline residues, which are essential for the conformational stability of mature collagen. Ethyl 3,4-dihydroxybenzoate (EDHB) is commonly used as a "P4H" inhibitor in cells, but suffers from low potency, poor selectivity, and off-target effects that cause iron deficiency. Dicarboxylates of 2,2'-bipyridine are among the most potent known CP4H inhibitors but suffer from a high affinity for free iron. A screen of biheteroaryl compounds revealed that replacing one pyridyl group with a thiazole moiety retains potency and enhances selectivity. A diester of 2-(5-carboxythiazol-2-yl)pyridine-5-carboxylic acid is bioavailable to human cells and inhibits collagen biosynthesis at concentrations that neither cause general toxicity nor disrupt iron homeostasis.
3.Down-regulation of collagen I biosynthesis in intestinal epithelial cells exposed to indomethacin: a comparative proteome analysis.
Edogawa S1, Sakai A2, Inoue T3, Harada S3, Takeuchi T3, Umegaki E3, Hayashi H2, Higuchi K3. J Proteomics. 2014 May 30;103:35-46. doi: 10.1016/j.jprot.2014.03.022. Epub 2014 Mar 31.
In contrast to accumulated knowledge about gastroduodenal injury associated with nonsteroidal antiinflammatory drugs (NSAIDs) such as indomethacin, small intestinal mucosal injuries have been noticed only recently, and the precise mechanism remains to be elucidated. To clarify the mechanism, we performed 2-DE on IEC-6 rat normal intestinal cells that were treated with indomethacin (200μΜ, 24h) or a vehicle control and identified 18 up-regulated and 8 down-regulated proteins through MALDI-TOF/TOF mass spectrometry. Among these proteins, collagen I and proteins involved in collagen I biosynthesis and maturation, including prolyl 4-hydroxylase subunit α1, protein disulfide isomerase A3 (PDIA3), calreticulin, and endoplasmin, were all down-regulated by indomethacin. Immunohistochemical staining of the intestinal mucosa of indomethacin-administered rats showed a decrease of collagen I on the apical surface of intestinal cells. Cell death induced by indomethacin was prominently suppressed when IEC-6 cells were grown on collagen I-coated plates.
4.The role of prolyl hydroxylase domain protein (PHD) during rosiglitazone-induced adipocyte differentiation.
Kim J1, Kwak HJ, Cha JY, Jeong YS, Rhee SD, Cheon HG. J Biol Chem. 2014 Jan 31;289(5):2755-64. doi: 10.1074/jbc.M113.493650. Epub 2013 Dec 12.
Rosiglitazone, a well known insulin sensitizer, stimulates adipocyte differentiation via the activation of peroxisome proliferator-activated receptor γ (PPARγ). Previous two-dimensional proteomics studies using C3H10T1/2 murine mesenchymal pluripotent stem cells revealed that prolyl hydroxylase domain protein (PHD) levels significantly increased during rosiglitazone-induced adipocyte differentiation (RIAD). In this study, we investigated the functional role played by PHD during RIAD. Three PHD isoforms (PHD1, 2, and 3) were found to be up-regulated in C3H10T1/2 cells during RIAD, whereas PHD knockdown and treatment with PHD inhibitors (dimethyloxalyl glycine or ethyl-3,4-dihydroxybenzoate) blocked RIAD. PHD inhibition was found to be associated with increases in the levels of anti-adipogenic proteins such as GATA-3, KLF-2, and transcriptional coactivator with PDZ binding motif (TAZ), with their reduced ubiquitination, suggesting that PHDs evoke the ubiquitination/proteasomal degradation of anti-adipogenic proteins.
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CAS 223666-07-7 Collagen proline hydroxylase inhibitor

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